Tetrahydroisoquinolines as MCH-R1 antagonists |
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Authors: | Sasikumar T K Qiang L Wu W-L Burnett D A Greenlee W J O'Neill K Hawes B E van Heek M Graziano M |
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Affiliation: | Schering-Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA. thavalakulamgar.sasikumar@spcorp.com |
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Abstract: | A series of potent and selective inhibitors of h-MCH-R1 has been developed based on the piperidine glycineamide compounds I and II. These structurally more rigid tetrahydroisoquinolines (III and IV) showed better pharmacokinetics. The highly potent compounds 12d and 12g displayed excellent rat pk. |
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